23536-76-7

Usage

Uses

Used in Pharmaceutical Industry:
7-Bromo-pyrido[1,2-a]pyrimidin-4-one is used as a key intermediate in the synthesis of various pharmaceutical compounds for the treatment of different diseases. Its unique structure allows for the development of new drugs with improved efficacy and selectivity.
Used in Drug Discovery and Development:
7-Bromo-pyrido[1,2-a]pyrimidin-4-one serves as a valuable building block in the design and synthesis of novel drug candidates. Its versatile chemical properties enable the creation of a wide range of biologically active molecules with potential therapeutic applications.
Used in Organic Chemistry Research:
7-BroMo-pyrido[1,2-a]pyriMidin-4-one is used as a model system in the study of chemical reactions and mechanisms in organic chemistry. Its unique structure provides insights into the reactivity and selectivity of various organic transformations, contributing to the advancement of chemical knowledge and techniques.

Upstream product

• 1072-97-5 5-bromo-2-pyridylamine 
• 25165-70-2 5-[(5-Bromo-pyridin-2-ylamino)-methylene]-2,2-dimethyl-[1,3]dioxane-4,6-dione 

Downstream Products

• 1848242-58-9 N-(5-{3-chloro-4-oxo-4H-pyrido[1,2-a]pyrimidin-7-yl}-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors

Aberrant signaling of fibroblast growth factor receptors (FGFRs) has been identified as a driver of tumorigenesis and the development of many solid tumors, making FGFRs a compelling target for anticancer therapy. Herein, we describe the design and synthes

Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR

The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.

PYRIDO[1,2-a]PYRIMIDONE DERIVATIVES AS A mTOR/PI3K SUPPRESSOR

The invention discloses pyrido[1,2-a]pyrimidone derivatives as a mTOR/PI3K suppressor; and in particular, this invention relates to a compound having the formula (I) structure or its pharmaceutically acceptable salts.

Synthesis of halogenated 4H-pyrido[1,2-a]pyrimidin-4-ones

Halogenated 4H-pyrido[l,2-a]pyrimidin-4-one were synthesized by thermal cyclization and decarboxylation of isopropylidene (2-pyridylamino)methylenemalonates, prepared from 2-aminopyridines and isopropylidene methoxymethylenemalonate formed in situ. Instead of 4H-pyrido[l,2-a]pyrimidin-4-ones, the 6-chloro and 6-bromo derivatives afforded mixtures of 7-halo-l,4-dihydro-l,8-naphthyridin-4-ones and 1-(6-halo-2-pyridyl)-3-[(6-halo-2-pyridylamino)methylene]-1,2,3,4-tetrahydropyridine-2,4-diones. The latters formed from N-(2-pyridyl)iminoketenes, the common intermediates of 4H-pyrido[l,2-a]pyrimidin-4-one and l,8-naphthyridin-4-ones, via a "head-to-tail" [4+2] cycloaddition. 3-Halo-4H-pyrido[l,2-a]pyrimidin-4-ones were obtained from 4H-pyrido[1,2-a]pyrimidin-4-one with N-halosuccinimides. The structures of the new compounds were characterized by means of 1H NMR and 13C NMR examinations.

Exotic amino acids. 6. Synthesis of substituted 4-oxo-4H-pyrido[1,2-a]pyrimidines

2-Pyridylaminomethyleneisopropylidenemalonates, prepared from ethoxymethyleneisopropylidenemalonate and 2-aminopyridines, form 4-oxo-4H-pyrido[1,2-a] pyrimidines at their melting points and are separated from the reaction mixture by sublimation.